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1.
Biochem Biophys Res Commun ; 705: 149743, 2024 04 23.
Artigo em Inglês | MEDLINE | ID: mdl-38442445

RESUMO

Neutrophil extracellular traps (NETs) released by neutrophils upon inflammation or infection, act as an innate immune defense against pathogens. NETs also influence inflammatory responses and cell differentiation in host cells. Osteoclasts, which are derived from myeloid stem cells, are critical for the bone remodeling by destroying bone. In the present study, we explores the impact of NETs, induced by the inflammatory agent calcium ionophore A23187, on the differentiation and activation of osteoclasts, potentially through suppressing RANK expression. Our results collectively suggested that the inhibition of RANKL-mediated osteoclastogenesis by NETs might lead to the suppression of excessive bone resorption during inflammation.


Assuntos
Reabsorção Óssea , Armadilhas Extracelulares , Humanos , Osteogênese , Osteoclastos , Neutrófilos , Diferenciação Celular , Inflamação , Ligante RANK
2.
Chembiochem ; 25(7): e202400013, 2024 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-38329925

RESUMO

Carboxylic polyether ionophores (CPIs) are among the most prevalent agricultural antibiotics (notably in the US) and these compounds have been in use for decades. The potential to reposition CPIs beyond veterinary use, e. g. through chemical modifications to enhance their selectivity window, is an exciting challenge and opportunity, considering their general resilience towards resistance development. Given the very large societal impact of these somewhat controversial compounds, it is surprising that many aspects of their mechanisms and activities in cells remain unclear. Here, we report comparative biological activities of the CPI routiennocin and two stereoisomers, including its enantiomer. We used an efficient convergent synthesis strategy to access the compounds and conducted a broad survey of antibacterial activities against planktonic cells and biofilms as well as the compounds' effects on mammalian cells, the latter assessed both via standard cell viability assays and broad morphological profiling. Interestingly, similar bioactivity of the enantiomeric pair was observed across all assays, strongly suggesting that chiral interactions do not play a decisive role in the mode of action. Overall, our findings are consistent with a mechanistic model involving highly dynamic behaviour of CPIs in biological membranes.


Assuntos
Antibacterianos , Policetídeos de Poliéter , Animais , Antibacterianos/farmacologia , Ionóforos/química , Mamíferos/metabolismo
3.
Cell Biol Toxicol ; 40(1): 26, 2024 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-38691186

RESUMO

Copper ionophore NSC319726 has attracted researchers' attention in treating diseases, particularly cancers. However, its potential effects on male reproduction during medication are unclear. This study aimed to determine whether NSC319726 exposure affected the male reproductive system. The reproductive toxicity of NSC319726 was evaluated in male mice following a continuous exposure period of 5 weeks. The result showed that NSC319726 exposure caused testis index reduction, spermatogenesis dysfunction, and architectural damage in the testis and epididymis. The exposure interfered with spermatogonia proliferation, meiosis initiation, sperm count, and sperm morphology. The exposure also disturbed androgen synthesis and blood testis barrier integrity. NSC319726 treatment could elevate the copper ions in the testis to induce cuproptosis in the testis. Copper chelator rescued the elevated copper ions in the testis and partly restored the spermatogenesis dysfunction caused by NSC319726. NSC319726 treatment also decreased the level of retinol dehydrogenase 10 (RDH10), thereby inhibiting the conversion of retinol to retinoic acid, causing the inability to initiate meiosis. Retinoic acid treatment could rescue the meiotic initiation and spermatogenesis while not affecting the intracellular copper ion levels. The study provided an insight into the bio-safety of NSC319726. Retinoic acid could be a potential therapy for spermatogenesis impairment in patients undergoing treatment with NSC319726.


Assuntos
Cobre , Espermatogênese , Testículo , Tretinoína , Masculino , Animais , Espermatogênese/efeitos dos fármacos , Tretinoína/farmacologia , Cobre/toxicidade , Camundongos , Testículo/efeitos dos fármacos , Testículo/metabolismo , Testículo/patologia , Espermatogônias/efeitos dos fármacos , Espermatogônias/metabolismo , Espermatozoides/efeitos dos fármacos , Espermatozoides/metabolismo , Meiose/efeitos dos fármacos , Epididimo/efeitos dos fármacos , Epididimo/metabolismo , Epididimo/patologia
4.
J Dairy Sci ; 107(2): 840-856, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-37730175

RESUMO

The objective of this study was to evaluate the effects of cashew nut shell extract (CNSE) and monensin on ruminal in vitro fermentation, CH4 production, and ruminal bacterial community structure. Treatments were as follows: control (CON, basal diet without additives); 2.5 µM monensin (MON); 0.1 mg CNSE granule/g DM (CNSE100); and 0.2 mg CNSE granule/g DM (CNSE200). Each treatment was incubated with 52 mL of buffered ruminal content and 500 mg of total mixed ration for 24 h using serum vials. The experiment was performed as a complete randomized block design with 3 runs. Run was used as a blocking factor. Each treatment had 5 replicates, in which 2 were used to determine nutrient degradability, and 3 were used to determine pH, NH3-N, volatile fatty acids, lactate, total gas, CH4 production, and bacterial community composition. Treatment responses for all data, excluding bacterial abundance, were analyzed with the GLIMMIX procedure of SAS v9.4. Treatment responses for bacterial community structure were analyzed with a PERMANOVA test run with the R package vegan. Orthogonal contrasts were used to test the effects of (1) additive inclusion (ADD: CON vs. MON, CNSE100, and CNSE200); (2) additive type (MCN: MON vs. CNSE100 and CNSE200); and (3) CNSE dose (DOS: CNSE100 vs. CNSE200). We observed that pH, acetate, and acetate:propionate ratio in the CNSE100 treatment were lower compared with CNSE200, and propionate in the CNSE100 treatment was greater compared with CNSE200. Compared with MON, CNSE treatments tended to decrease total lactate concentration. Total gas production of CON was greater by 2.63% compared with all treatments, and total CH4 production was reduced by 10.64% in both CNSE treatments compared with MON. Also, compared with MON, in vitro dry matter degradabilities in CNSE treatments were lower. No effects were observed for NH3-N or in vitro neutral detergent fiber degradability. Finally, the relative abundances of Prevotella, Treponema, and Schwartzia were lower, whereas the relative abundances of Butyrivibrio and Succinivibrio were greater in all treatments compared with CON. Overall, the inclusion of CNSE decreased CH4 production compared with MON, making CNSE a possible CH4 mitigation additive in dairy cattle diets.


Assuntos
Anacardium , Monensin , Bovinos , Feminino , Animais , Monensin/farmacologia , Monensin/metabolismo , Lactação , Propionatos/metabolismo , Fermentação , Nozes , Digestão , Dieta/veterinária , Bactérias , Acetatos/farmacologia , Metano/metabolismo , Lactatos/metabolismo , Extratos Vegetais/farmacologia , Rúmen/metabolismo , Ração Animal/análise
5.
Parasitol Res ; 123(2): 139, 2024 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-38381180

RESUMO

The flow of calcium ions (Ca2+) is involved in numerous vital activities of Toxoplasma gondii. Calreticulin is a type of Ca2+-binding protein in the endoplasmic reticulum (ER) that is involved in Ca2+ signaling pathway regulation, Ca2+ storage, and protein folding. In this work, the calreticulin (CALR), a protein predicted to possess a conserved domain of calreticulin in T. gondii, was characterized. The CALR localized in the ER. Using reverse genetics, we discovered that CALR is not necessary for the lytic cycle, including invasion and replication. However, depletion of CALR affected microneme secretion triggered by A23187, which is a Ca2+ ionophore used to increase cytoplasmic Ca2+ concentration. Furthermore, we discovered that CALR influences Ca2+ release. Transcriptomic comparison between Δcalr and Δku80 parasites showed that 226 genes in the Δcalr parasites were significantly downregulated (p < 0.05). The cellular biological functions of the downregulated genes were mainly involved in calmodulin-dependent protein kinase pathways. Furthermore, in the absence of CALR, tachyzoites were still able to cause acute infection in mice. These results imply that by influencing ER Ca2+ release content, CALR may further impair the ionophore-induced secretion of the parasite. However, this protein is not required for the completion of the parasite's lytic cycle or for the acute virulence of the parasite.


Assuntos
Calreticulina , Proteínas de Protozoários , Toxoplasma , Animais , Camundongos , Calreticulina/genética , Calreticulina/metabolismo , Retículo Endoplasmático , Ionóforos , Micronema , Toxoplasma/genética , Toxoplasma/metabolismo , Proteínas de Protozoários/genética , Proteínas de Protozoários/metabolismo
6.
Mikrochim Acta ; 191(8): 467, 2024 Jul 18.
Artigo em Inglês | MEDLINE | ID: mdl-39023534

RESUMO

PdRuO2/PVP nanomaterial was synthesized using a straightforward method and characterized using advanced analytical methods such as TEM, XRD, XPS, elemental mapping and SEM. The synthesized PdRuO2/PVP nanomaterial was used as an ionophore in potentiometric sensor electrodes and successfully adapted to Cr3+ ion detection in a large number of aqueous samples. Several experimental parameters of the PdRuO2/PVP sensor such as potentiometric behavior, selectivity, repeatability, response time, pH, titration, and recovery in real samples were investigated. Potentiometric behavioral characteristics were performed in the concentration range 1 × 10-6-1.0 × 10-1 M. The repeated experiments performed six times showed that there was no deviation in the measurements. The limit of detection of the PdRuO2/PVP potentiometric sensor was very low with a value of 8.6 × 10-8 M. The potentiometric measurements showed that the synthesized PdRuO2/PVP ionophore was highly effective in detecting Cr3+ in a wide pH range of 2.0-8.0 and was found to have a shelf life of over 1 year. As a result, the synthesized PdRuO2/PVP electrode material was found to be highly selective, stable, and applicable for Cr3+ detection.

7.
Molecules ; 29(13)2024 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-38999058

RESUMO

The commercial veterinary antibiotic sodium monensinate (MonNa) binds mercury(II) or zinc(II) cations as thiocyanate [Hg(MonNa)2(SCN)2] (1) or isothiocyanate [Zn(MonNa)2(NCS)2] (2) neutral coordination compounds. The structure and physicochemical properties of 1 and 2 were evaluated by the methods of single crystal and/or powder X-ray diffraction, infrared, nuclear magnetic resonance, X-ray photoelectron spectroscopies, and electrospray-mass spectrometry. The primary cores of the two complexes comprise HgS2O2 (1) and ZnN2O2 (2) coordination motifs, respectively, due to the ambidentate binding modes of the SCN-ligands. The directly bound oxygen atoms originate from the carboxylate function of the parent antibiotic. Sodium cations remain in the hydrophilic cavity of monensin and cannot be replaced by the competing divalent metal ions. Zinc(II) binding does not influence the monensin efficacy in the case of Bacillus cereus and Staphylococcus aureus whereas the antimicrobial assay reveals the potential of complex 2 as a therapeutic candidate for the treatment of infections caused by Bacillus subtilis, Kocuria rhizophila, and Staphylococcus saprophyticus.


Assuntos
Complexos de Coordenação , Mercúrio , Zinco , Zinco/química , Complexos de Coordenação/química , Complexos de Coordenação/farmacologia , Mercúrio/química , Ligantes , Antibacterianos/farmacologia , Antibacterianos/química , Testes de Sensibilidade Microbiana , Cristalografia por Raios X , Estrutura Molecular
8.
AAPS PharmSciTech ; 25(5): 104, 2024 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-38724836

RESUMO

Salinomycin (Sal) has been recently discovered as a novel chemotherapeutic agent against various cancers including prostate cancer which is one of the most commonly diagnosed cancers affecting male populations worldwide. Herein we designed salinomycin nanocarrier (Sal-NPs) to extend its systemic circulation and to increase its anticancer potential. Prepared nanoform showed high encapsulation and sustained release profile for salinomycin. The present study elucidated the cytotoxicity and mechanism of apoptotic cell death of Sal-NPs against prostate cancer both in vitro and in vivo. At all measured concentrations, Sal-NPs showed more significant cytotoxicity to DU145 and PC3 cells than Sal alone. This effect was mediated by apoptosis, as confirmed by ROS generation, loss of MMP and cell cycle arrest at the G1 phase in both cells. Sal-NPs efficiently inhibited migration of PC3 and DU145 cells via effectively downregulating the epithelial mesenchymal transition. Also, the results confirmed that Sal-NPs can effectively inhibit the induction of Prostate adenocarcinoma in male Wistar rats. Sal-NPs treatment exhibited a decrease in tumour sizes, a reduction in prostate weight, and an increase in body weight, which suggests that Sal-NPs is more effective than salinomycin alone. Our results suggest that the molecular mechanism underlying the Sal-NPs anticancer effect may lead to the development of a potential therapeutic strategy for treating prostate adenocarcinoma.


Assuntos
Adenocarcinoma , Antineoplásicos , Apoptose , Portadores de Fármacos , Transição Epitelial-Mesenquimal , Nanopartículas , Neoplasias da Próstata , Piranos , Ratos Wistar , Masculino , Neoplasias da Próstata/tratamento farmacológico , Neoplasias da Próstata/patologia , Neoplasias da Próstata/metabolismo , Animais , Piranos/farmacologia , Piranos/administração & dosagem , Apoptose/efeitos dos fármacos , Humanos , Ratos , Linhagem Celular Tumoral , Adenocarcinoma/tratamento farmacológico , Adenocarcinoma/patologia , Adenocarcinoma/metabolismo , Portadores de Fármacos/química , Nanopartículas/química , Transição Epitelial-Mesenquimal/efeitos dos fármacos , Antineoplásicos/farmacologia , Antineoplásicos/administração & dosagem , Movimento Celular/efeitos dos fármacos , Células PC-3 , Sistemas de Liberação de Medicamentos/métodos , Policetídeos de Poliéter
9.
Chemistry ; 29(54): e202203323, 2023 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-37385951

RESUMO

As shown by IncuCyte Zoom imaging proliferation assays, invasive triple-negative human breast MDA-MB-231 cancer cells treated with sub-toxic doses (5.0-20 µM, 72 h) of [GaQ3 ] (Q=8-hydroxyquinolinato) caused profound morphological changes and inhibition of cell migration, which were likely due to terminal cell differentiation or similar phenotypical change. This is the first demonstration of potential use of a metal complex in differentiation anti-cancer therapy. Additionally, a trace amount of Cu(II) (0.20 µM) added to the medium dramatically increased [GaQ3 ] cytotoxicity (IC50 ~2 µM, 72 h) due to its partial dissociation and the action of the HQ ligand as a Cu(II) ionophore, as shown with electrospray mass spectrometry and fluorescence spectroscopy assays in the medium. Hence, cytotoxicity of [GaQ3 ] is strongly linked to ligand binding of essential metal ions in the medium, for example, Cu(II). Appropriate delivery mechanisms of such complexes and their ligands could enable a powerful new triple therapeutic approach for cancer chemotherapy, including cytotoxicity against primary tumour, arrest of metastases, and activation of innate and adaptive immune responses.


Assuntos
Antineoplásicos , Complexos de Coordenação , Humanos , Cobre/química , Ligantes , Antineoplásicos/farmacologia , Antineoplásicos/química , Complexos de Coordenação/química , Metais/farmacologia , Proliferação de Células , Linhagem Celular Tumoral
10.
Mol Cell Biochem ; 478(12): 2683-2693, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36914880

RESUMO

Heavy metal ions are essential micronutrients for human health. They are also indispensable to maintaining health and regular operation of organs. Increasing or decreasing these metal ions will lead to cell death, such as ferroptosis. Tsvetkov et al. have recently proposed a novel cell death method called "Cuproptosis". Many researchers have linked this form of death to the diagnosis, prognosis, microenvironment infiltration, and prediction of immunotherapeutic efficacy of various tumors to better understand these tumors. Similarly, with the proposal of this mechanism, the killing effect of copper ionophores on cancer cells has come to our attention again. We introduced the mechanism of cuproptosis in detail and described the establishment of the corresponding prognostic model and risk score for uveal melanoma through cuproptosis. In addition, we describe the current progress in the study of cancer in other organs through cuproptosis and summarize the treatment of tumours by copper ionophore and its future research direction. With further research, the concept of cuproptosis may help us understand cancer and guide its clinical treatment.


Assuntos
Melanoma , Neoplasias Uveais , Humanos , Cobre , Morte Celular , Ionóforos , Íons , Apoptose , Microambiente Tumoral
11.
Anal Bioanal Chem ; 415(18): 4233-4243, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-36045175

RESUMO

We present here an ionophore-based ion-selective optode (ISO) platform to detect potassium and sodium concentrations in serum through flow cytometry. The ion-selective microsensors were based on polyethylene glycol (PEG)-modified polystyrene (PS) microspheres (PEG-PS). Ratiometric response curves were observed using peak channel fluorescence intensities for K+ (10-6 M to 0.1 M) and Na+ (10-4 M to 0.2 M) with sufficient selectivity for clinical diagnosis. Due to the matrix effect, proteins such as albumin and immunoglobulin caused an obvious increase in response for serum sample determination. To solve this problem, 4-arm PEG chains were covalently attached onto the surface of PS microspheres through a two-step reaction, which improved the stability and combated pollution of microspheres. As a preliminary application, potassium and sodium concentrations in human serums were successfully determined by the PEG-PS microsensors through flow cytometry.


Assuntos
Polietilenoglicóis , Potássio , Humanos , Microesferas , Citometria de Fluxo , Ionóforos , Íons , Sódio
12.
Zygote ; 31(1): 85-90, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36515071

RESUMO

The objective of this study was to assess the effects of pentoxifylline (PTX) and Ca2+ ionophore (CI) A12387 treatment on some biological characteristics of sperm cells in oligoasthenoteratozoospermia (OAT) patients. After processing, each sample was divided into four groups: 1, control; 2, exposed to 3.6 mM PTX; 3, exposed to 5 µm calcium ionophore (CI); and 4, exposed to both PTX and CI; 30 min at 37°C. Sperm motility was measured before and after preparation. Acrosome reaction (AR), status of sperm vacuoles, mitochondrial membrane potential (MMP) and DNA fragmentation were assessed using PSA-FITC staining, motile sperm organelle morphology examination (MSOME), JC-1 staining and sperm chromatin dispersion (CSD) test, respectively. Treatment with PTX and CI led to increased and decreased sperm motility, respectively (P < 0.05). Furthermore, vacuole status and rates of sperm DNA fragmentation were not significantly different among groups (P > 0.05). Moreover, the data showed that the rates of AR and disrupted MMP were significantly different between groups (P < 0.05). In conclusion, in vitro application of PTX not only did not have any adverse effects on sperm cell biology characteristics, but also can rectify the harmful effect of CI.


Assuntos
Astenozoospermia , Infertilidade Masculina , Oligospermia , Pentoxifilina , Masculino , Humanos , Pentoxifilina/farmacologia , Pentoxifilina/metabolismo , Oligospermia/tratamento farmacológico , Oligospermia/metabolismo , Ionóforos de Cálcio/farmacologia , Ionóforos de Cálcio/metabolismo , Astenozoospermia/tratamento farmacológico , Astenozoospermia/metabolismo , Sêmen , Infertilidade Masculina/terapia , Motilidade dos Espermatozoides , Espermatozoides
13.
Sensors (Basel) ; 23(6)2023 Mar 16.
Artigo em Inglês | MEDLINE | ID: mdl-36991892

RESUMO

The saltiness enhancement effect can be produced by adding specific substances to dietary salt (sodium chloride). This effect has been used in salt-reduced food to help people forge healthy eating habits. Therefore, it is necessary to objectively evaluate the saltiness of food based on this effect. In a previous study, sensor electrodes based on lipid/polymer membrane with Na+ ionophore have been proposed to quantify the saltiness enhanced by branched-chain amino acids (BCAAs), citric acid, and tartaric acid. In this study, we developed a new saltiness sensor with the lipid/polymer membrane to quantify the saltiness enhancement effect of quinine by replacing a lipid that caused an unexpected initial drop in the previous study with another new lipid. As a result, the concentrations of lipid and ionophore were optimized to produce an expected response. Logarithmic responses have been found on both NaCl samples and quinine-added NaCl samples. The findings indicate the usage of lipid/polymer membranes on novel taste sensors to evaluate the saltiness enhancement effect accurately.

14.
Int J Mol Sci ; 24(2)2023 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-36675211

RESUMO

For many years, ionophores have been used to control coccidiosis in poultry. However, misuse of ionophores can cause toxicity with significant clinical symptoms. The most critical factors influencing ionophores' toxicity are administration dose, species, and animal age. Although clinical signs of ionophore intoxication are well studied, the toxicity mechanisms of the ionophores at the molecular level still are not fully elucidated. This review summarizes the studies focused on polyether ionophores toxicity mechanisms in animals at the clinical and molecular levels. Studies show that ionophore toxicity mainly affects myocardial and skeletal muscle cells. The molecular mechanism of the toxication could be explained by the inhibition of oxidative phosphorylation via dysregulation of ion concentration. Tiamulin-ionophore interaction and the synergetic effect of tiamulin in ionophore biotransformation are discussed. Furthermore, in recent years ionophores were candidates for reprofiling as antibacterial and anti-cancer drugs. Identifying ionophores' toxicity mechanisms at the cellular level will likely help develop novel therapies in veterinary and human medicine.


Assuntos
Antibacterianos , Coccidiose , Animais , Humanos , Ionóforos/farmacologia , Ionóforos/metabolismo , Antibacterianos/metabolismo , Aves Domésticas/metabolismo
15.
Int J Mol Sci ; 24(24)2023 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-38139286

RESUMO

Quercetin forms complexes with various metals due to its structural attributes. It predominantly exhibits chelating activity at the 3-hydroxy/4-carbonyl group. Previously, coordination in synthetically obtained quercetin-zinc (II) complexes has been limited to this group. However, the expanded coordination observed in quercetin-iron complexes has opened avenues for diverse applications. Thus, synthesizing novel quercetin-zinc complexes with different coordination positions is a significant advance. In our study, we not only synthesized and comprehensively characterized a new quercetin-zinc (II) complex, Zn-Q, but also evaluated the structure and bioactivity of chelate complexes (Q+Zn) derived from co-treatment in cell culture mediums. The structure of the new compound Zn-Q was comprehensively characterized using 1D 1H and 2D correlation spectroscopy (COSY), nuclear magnetic resonance (NMR), Fourier-transform infrared spectroscopy (FT-IR), ultraviolet-visible spectroscopy (UV-Vis), electrospray ionization mass spectrometer (ESI-MS), and X-ray diffraction analysis (XRD) analysis. Subcellular localization and absorption of these zinc (II) complexes were determined using the ZnAF-2 DA zinc ion fluorescence probe. Throughout the experiments, both Zn-Q and Q+Zn exhibited significant antioxidant, cell growth inhibitory, and anticancer effects in HepG2 and HCT116 cells, with Zn-Q showing the highest potential for inducing apoptosis via the caspase pathway. Tracking intracellular zinc complex absorption using zinc fluorescent probes revealed zinc (II) localization around the cell nucleus. Interestingly, there was a proportional increase in intracellular quercetin absorption in conjunction with zinc (II) uptake. Our research highlights the advantages of quercetin complexation with zinc (II): enhanced anticancer efficacy compared to the parent compound and improved bioavailability of both quercetin and zinc (II). Notably, our findings, which include enhanced intracellular uptake of both quercetin and zinc (II) upon complex formation and its implications in apoptosis, contribute significantly to the understanding of metal-polyphenol complexes. Moving forward, comprehensive functional assessments and insights into its mechanism of action, supported by animal studies, are anticipated.


Assuntos
Complexos de Coordenação , Zinco , Humanos , Animais , Zinco/química , Quercetina/farmacologia , Quercetina/química , Células HCT116 , Espectroscopia de Infravermelho com Transformada de Fourier , Complexos de Coordenação/farmacologia , Complexos de Coordenação/química , Apoptose
16.
Molecules ; 28(24)2023 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-38138575

RESUMO

A series of five esters of lasalocid with neopentyl alcohol (LasNeo), geraniol (LasGeran), 2-ethylhexanol (LasEtHex), eicosanol (LasEico) and vanillyl alcohol (LasVanil) were synthesized and studied by NMR, FT-IR and ESI-MS. Then, their complexes with lithium, sodium and potassium cations were obtained and examined using FT-IR. The analysis of the products confirmed the synthesis of new esters with good yields. The newly obtained compounds, as well as their complexes with monovalent cations, were proved to be stabilized by a strong system of intramolecular hydrogen bonds. The PM6 semiempirical calculations provided information on the heat of formation (HOF) and permitted the making of visual representations of the structures of the newly synthesized esters and their complexes with the investigated cations. All the computational outcomes were consistent with the spectroscopic data.

17.
Molecules ; 28(22)2023 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-38005274

RESUMO

Gemcitabine is a chemotherapeutic agent used to treat various malignancies, including breast and bladder cancer. In the current study, three innovative selective gemcitabine hydrochloride sensors are developed using 4-tert-butylcalix-[8]-arene (sensor 1), ß-cyclodextrin (sensor 2), and γ-cyclodextrin (sensor 3) as ionophores. The three sensors were prepared by incorporating the ionophores with o-nitrophenyl octyl ether as plasticizer and potassium tetrakis(4-chlorophenyl) borate as ionic additive into a polyvinyl chloride polymer matrix. These sensors are considered environmentally friendly systems in the analytical research. The linear responses of gemcitabine hydrochloride were in the concentration range of 6.0 × 10-6 to 1.0 × 10-2 mol L-1 and 9.0 × 10-6 to 1.0 × 10-2 mol L-1 and 8.0 × 10-6 to 1.0 × 10-2 mol L-1 for sensors 1, 2, and 3, respectively. Over the pH range of 6-9, fast-Nernst slopes of 52 ± 0.6, 56 ± 0.3, and 55 ± 0.8 mV/decade were found in the same order with correlation regressions of 0.998, 0.999, and 0.998, respectively. The lower limits of detection for the prepared sensors were 2.5 × 10-6, 2.2 × 10-6, and 2.7 × 10-6 mol L-1. The sensors showed high selectivity and sensitivity for gemcitabine. Validation of the sensors was carried out in accordance with the requirements established by the IUPAC, while being inexpensive and easy to use in drug formulation. A statistical analysis of the methods in comparison with the official method showed that there was no significant difference in accuracy or precision between them. It was shown that the new sensors could selectively and accurately find gemcitabine hydrochloride in bulk powder, pharmaceutical formulations, and quality control tests. The ionophore-based sensor shows several advantages over conventional PVC membrane sensor sensors regrading the lower limit of detection, and higher selectivity towards the target ion.


Assuntos
Antineoplásicos , Gencitabina , Composição de Medicamentos , Ionóforos , Polímeros , Potenciometria/métodos , Cloreto de Polivinila
18.
Molecules ; 28(10)2023 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-37241883

RESUMO

Unlike conventional lead ion (Pb2+) detecting methods, electrochemical methods have the attractive advantages of rapid response, good portability and high sensitivity. In this paper, a planar disk electrode modified by multiwalled carbon nanotube (MWCNTs)/chitosan (CS)/lead (Pb2+) ionophore IV nanomaterial and its matched system are proposed. This system presented a good linear relationship between the concentration of Pb2+ ions and the peak current in differential pulse stripping voltammetry (DPSV), under optimized conditions of -0.8 V deposition potential, 5.5 pH value, 240 s deposition time, performed sensitive detection of Pb2+ within sensitivity of 1.811 µA · µg-1 and detection limit of 0.08 µg · L-1. Meanwhile, the results of the system in detecting lead ions in real seawater samples are highly similar to that of inductively coupled plasma emission spectrometer (ICP-MS), which proved a practicability for the system in detection of trace-level Pb2+.

19.
Molecules ; 28(12)2023 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-37375231

RESUMO

The largely uncharted complexation chemistry of the veterinary polyether ionophores, monensic and salinomycinic acids (HL) with metal ions of type M4+ and the known antiproliferative potential of antibiotics has provoked our interest in exploring the coordination processes between MonH/SalH and ions of Ce4+. (1) Methods: Novel monensinate and salinomycinate cerium(IV)-based complexes were synthesized and structurally characterized by elemental analysis, a plethora of physicochemical methods, density functional theory, molecular dynamics, and biological assays. (2) Results: The formation of coordination species of a general composition [CeL2(OH)2] and [CeL(NO3)2(OH)], depending on reaction conditions, was proven both experimentally and theoretically. The metal(IV) complexes [CeL(NO3)2(OH)] possess promising cytotoxic activity against the human tumor uterine cervix (HeLa) cell line, being highly selective (non-tumor embryo Lep-3 vs. HeLa) compared to cisplatin, oxaliplatin, and epirubicin.


Assuntos
Cério , Monensin , Humanos , Monensin/farmacologia , Monensin/química , Cério/farmacologia , Ionóforos/química , Íons
20.
Molecules ; 28(6)2023 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-36985781

RESUMO

A novel amperometric sensor for the direct determination of toxic mercury ions, Hg2+, based on the organic chelator ionophore N, N di (2-hydroxy-5-[(4-nitrophenyl)diazenyl]benzaldehyde) benzene-1,2-diamine (NDBD), and multiwalled carbon nanotubes (MWCNT) immobilized on a glassy carbon electrode surface was developed. The parameters influencing sensor performance including the ionophore concentration, the applied potential, and electrolyte pH were optimized. The sensor response to Hg2+ was linear between 1-25 µM with a limit of detection of 60 nM. Interferences from other heavy metal ions were evaluated and the sensor showed excellent selectivity towards Hg2+. The method was successfully applied to the determination of mercury ions in milk and water samples.

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